Polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) micelles for paclitaxel delivery

Physicochemical properties of two anhydrates (α-form and β-form) and three hydrates (hemihydrate, monohydrate and sesquihydrate) of sitafloxacin (STFX), a novel fluoroquinolone antibiotic, were investigated and correlated with the crystal structure of each crystalline form. STFX sesquihydrate showed larger weight change between 1% and 95% relative humidities (RHs) than other crystalline forms. In the crystal of sesquihydrate, STFX molecules form a channel structure where water molecules exist. Contrary to sesquihydrate, water molecules in a monohydrate are located in well-defined and isolated crystallographic sites. The β-form exhibited the worst photostability than any other forms under the irradiation of a D65 lamp. The intramolecular hydrogen bonding in the β-form caused a red shift on the solid-state UV spectrum by prolonging the conjugation system of the quinolone ring, resulting in greater absorption of photoenergy and consequent degradation. Solubility is also affected by the crystalline structure. Standard free energy of the formation of STFX molecule in each crystalline form and/or lattice energy binding STFX molecules to retain the crystal structure might cause a difference in solubility.     

Paclitaxel-loaded polymeric micelles based on poly(ɛ-caprolactone)-poly(ethylene glycol)-poly(ɛ-caprolactone) triblock copolymers: in vitro and in vivo evaluation

The purpose of this study was to develop polymeric nanoscale drug-delivery system (nano-DDS) for paclitaxel (PTX) from poly(?-caprolactone)-poly(ethylene glycol)-poly(?-caprolactone) (PCL-PEG-PCL, PCEC) copolymers, intended to be intravenously administered, able to improve the therapeutic efficacy of the drug and devoid of the adverse effects of Cremophor EL. Both of the PTX-loaded polymeric micelles and polymersomes were successfully prepared from PCEC copolymers. The obtained PTX-loaded micelles exhibited core-shell morphology with satisfactory size (93 nm), and were favorable for intravenous injection. In vitro cytotoxicity demonstrated that the cytotoxic effect of PTX-loaded micelles was lower than that of Taxol (Bristol-Myers Squibb, Princeton, New Jersey). Pharmacokinetic results indicated that the PTX-loaded micelles had longer systemic circulation time and slower plasma elimination rate than those of Taxol. Furthermore, PTX-loaded micelles showed greater tumor growth-inhibition effect in vivo on EMT6 breast tumor, in comparison with Taxol. Therefore, the prepared polymeric micelles might be potential nano-DDS for PTX delivery in cancer chemotherapy.From the Clinical EditorIn this paper, a paclitaxel- loaded polymeric micelle system is demonstrated to provide optimized intravenous delivery method of this anti-cancer agent. While the study is early preclinical, this approach may have the potential to eventually be studied in clinical trials as well.     

Functionalized (poly(ɛ-caprolactone))₂-poly(ethylene glycol) nanoparticles with grafting nicotinic acid as drug carriers

Nicotinic acid was grafted on (poly(?-caprolactone))₂-poly(ethylene glycol) copolymers that were used for the preparation of nanoparticles with the objectives to monitor particle size and to optimize the drug loading capacity as well as the release profile of the particles. Increasing amounts of grafting nicotinic acid increased the particle size as a result of an enhanced hydrophobicity of the copolymer. Ibuprofen and indomethacin with two different molecular characteristics were selected as model drugs to be bound to the nanoparticles. The presence of grafting nicotinic acid enhanced the loading capacity for both drugs compared to the nanoparticles without nicotinic acid. However, no correlation between amount of grafting nicotinic acid and loading capacity was observed. The release characteristic of both drugs was fitted to the Higuchi model indicating Fickian diffusion. The release characteristic of indomethacin mainly depended on the crystalline property of the copolymer whereas that of ibuprofen was additionally influenced by the hydrogen bonding between drug and grafted copolymer.     

Antibacterial electrospun poly(ɛ-caprolactone)/ascorbyl palmitate nanofibrous materials

The one-step incorporation of ascorbyl palmitate (AP), a widely used derivative of vitamin C, into nanofibrous mats of poly(?-caprolactone) (PCL) by electrospinning was demonstrated. The incorporation of AP was attested by IR spectroscopy; the AP content was determined by thermogravimetric analysis (TGA); and the surface composition of the mats: by X-ray photoelectron spectroscopy (XPS). The possibility for deposition of silver nanoparticles onto PCL/AP mats using the ability of AP to reduce silver ions was demonstrated. The silver content was determined by TGA, and the silver nanoparticles were observed by transmission electron microscopy (TEM). The nanoparticles were composed of elemental silver, as verified by XPS analyses. The UV-vis spectrophotometric analyses, study on quenching of the free 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and microbiological tests against the pathogenic microorganism Staphylococcus aureus showed that AP preserved its stability and its antioxidant and antibacterial activity when incorporated in the nanofibrous mats.     

Biodegradable poly(ɛ-caprolactone)–poly(ethylene glycol) copolymers as drug delivery system

Poly(?-caprolactone)–poly(ethylene glycol) (PCL–PEG) copolymers are important synthetic biomedical materials with amphiphilicity, controlled biodegradability, and great biocompatibility. They have great potential application in the fields of nanotechnology, tissue engineering, pharmaceutics, and medicinal chemistry. This review introduced several aspects of PCL–PEG copolymers, including synthetic chemistry, PCL–PEG micro/nanoparticles, PCL–PEG hydrogels, and physicochemical and toxicological properties.     

Growth factor releasing porous poly (ɛ-caprolactone)-chitosan matrices for enhanced bone regenerative rherapy

Drug releasing porous poly(epsilon-caprolactone) (PCL)-chitosan matrices were fabricated for bone regenerative therapy. Porous matrices made of biodegradable polymers have been playing a crucial role as bone substitutes and as tissue-engineered scaffolds in bone regenerative therapy. The matrices provided mechanical support for the developing tissue and enhanced tissue formation by releasing active agent in controlled manner. Chitosan was employed to enhance hydrophilicity and biocompatibility of the PCL matrices. PDGF-BB was incorporated into PCL-chitosan matrices to induce enhanced bone regeneration efficacy. PCL-chitosan matrices retained a porous structure with a 100-200 microm pore diameter that was suitable for cellular migration and osteoid ingrowth. NaHCO3 as a porogen was incorporated 5% ratio to polymer weight to form highly porous scaffolds. PDGF-BB was released from PCL-chitosan matrices maintaining therapeutic concentration for 4 week. High osteoblasts attachment level and proliferation was observed from PCL-chitosan matrices. Scanning electron microscopic examination indicated that cultured osteoblasts showed round form and spread pseudopods after 1 day and showed broad cytoplasmic extension after 14 days. PCL-chitosan matrices promoted bone regeneration and PDGF-BB loaded matrices obtained enhanced bone formation in rat calvarial defect. These results suggested that the PDGF-BB releasing PCL-chitosan porous matrices may be potentially used as tissue engineering scaffolds or bone substitutes with high bone regenerative efficacy.     

Poly(ethylene glycol)-poly(ε-caprolactone) Iodinated Nanocapsules as Contrast Agents for X-ray Imaging

Purpose

Synthesis and formulation of iodinated PCL-mPEG nanocapsules as new original blood pool contrast agents for computed tomography.

Methods

PCL-mPEG was synthesized and formulated following the emulsion–solvent diffusion process, in the form of iodinated nanocapsules. Physico-chemical characterization of such nano-materials was performed by DLS and transmission electron microscopy. A stability study of the nanocapsules suspension was followed-up to 3 month. Blood biocompatibility was performed. Finally, the nanocapsules suspension radiopacity was evaluated in vitro then in vivo in mice as micro-CT contrast agent.

Results

In this study, the iodine concentration in nanocapsules suspension was about 70 mgI/mL. Besides, these nanocarriers appeared non-toxic, and stable in suspension. In vivo, i.v. administration of 10 μL/g of mouse body weight of theses nano-particles induced a vascular contrast enhancement of 168 HU and a half-life in blood of 4.2 +/? 0.5 h. Elimination route of these particles appears mainly performed by the liver, without sequestration in spleen and lymph nodes confirming their stealth properties.

Conclusions

This study proposes the first example of iodinated biodegradable polymeric blood pool contrast agent, able to induce an exploitable contrast enhancement. The main advantage of polymeric system compared to lipid ones, lies in their stability and handling, e.g. towards drying for storage.     

In vivo cancer imaging by poly(ethylene glycol)-b-poly(ɛ-caprolactone) micelles containing a near-infrared probe

Noninvasive near-infrared (NIR) fluorescence imaging is a promising technique for the intraoperative assessment of solid tumor removal. We incorporated a lipophilic NIR probe, 1,1′-dioctadecyltetramethyl indotricarbocyanine iodide (DiR), in poly(ethylene glycol)-b-poly(?-caprolactone) (PEG-b-PCL) micelles, resulting in DiR solubilization in water, occupying nanoscopic PEG-b-PCL micelles. DiR in a self-quenched or nonquenched state showed different kinetics of release from PEG-b-PCL micelles in vitro; however, both obtained high tumor delineation (tumor-to-muscle ratio of 30–43 from collected organs). These results suggest that PEG-b-PCL micelles with DiR are a promising nanosized imaging agent that will provide a basis for enhanced surgical guidance via NIR visualization of tumors.From the Clinical EditorIn this paper, noninvasive near-infrared fluorescence imaging coupled with specific lipophilic probes is discussed as a promising technique for intraoperative assessment of solid tumor removal, leading to optimized outcomes for in toto removal of tumors.     

Enhanced anti-glioblastoma efficacy by PTX-loaded PEGylated poly(ɛ-caprolactone) nanoparticles: In vitro and in vivo evaluation

The aim of this work was to investigate the anti-tumor effect of paclitaxel (PTX)-loaded methoxy poly(ethylene glycol)-poly(?-caprolactone) nanoparticles (MPEG-NP/PTX) against glioblastoma multiforme (GBM). MPEG-NP/PTX was prepared by the emulsion and evaporation technique with particle size of 72.5±2.2nm and did not change remarkably during the period of 21-day storage at 4°C. The drug-loading coefficient and encapsulation ratio of optimized formulation were 8.2±0.6% and 90.4±2.3%, respectively. The in vitro release behavior exhibits a biphase release manner and was affected by PEG segment. In vitro cytotoxicity was assessed using C6 cell lines and was compared to Taxol and PTX-loaded poly(?-caprolactone) conventional nanoparticles (NP/PTX). Cell viability assay against C6 cells exhibited higher or at least comparable cytotoxicity than that of Taxol and NP/PTX. More importantly, in vivo real-time fluorescence imaging analysis in intracranial C6 glioblastoma bearing mice showed that the methoxy poly(ethylene glycol)-poly(?-caprolactone) nanoparticles (MPEG-NP) displayed much stronger fluorescence signal and 3-fold larger Area-Under-Curve (AUC) than poly(?-caprolactone) conventional nanoparticles (NP) in tumor-bearing brain. Furthermore, in vivo anti-glioblastoma effect exhibited the mean survive time of MPEG-NP/PTX (28 days) was much longer than those of Taxol injection (20 days) and NP/PTX (23 days). Therefore, MPEGylated poly(?-caprolactone) nanoparticles significantly enhanced the anti-glioblastoma activity of PTX and might be considered a promising drug delivery system against advanced glioblastoma.     

Treatments of paclitaxel with poly(vinyl pyrrolidone) to improve drug release from poly(ɛ-caprolactone) matrix for film-based stent

Drug-loaded biodegradable films as a principal part of film-based stent were investigated for controlled drug delivery systems. In this study, solid dispersion technique, a pretreatment method of paclitaxel (PTX), was applied to prepare the PTX-loaded poly(?-caprolactone) (PCL) films. Drug dissolution rates and characteristics of the poly(vinyl pyrrolidone) (PVP)/PTX solid dispersions (SDs) and physical mixtures (PMs) were investigated to show that the PVP/PTX SDs were successfully prepared before being incorporated in biodegradable films. Afterwards, the effect of the application of SDs on improving drug release behavior, weightlessness, crystalline states, and surface and internal morphologies of the films were studied. It was found that, the films with SDs showed a higher drug release rate than the films with PMs or pure PTX. In addition, the content of PVP in the SDs also had impact on drug release behavior: the more PVP in SDs, the faster the drug was released. According to the drug release test and weightlessness study, the possible drug release mechanism was put forward for the films with SDs. The application of solid dispersion technique showed a remarkable effect on improving drug release behavior for film-based biodegradable stent drug delivery systems.     

Hemocompatibility of poly(ɛ-caprolactone) lipid-core nanocapsules stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan

Optimum experimental parameters for modulated differential scanning calorimetry were determined using a design of experiments approach. Two different strategies were tested, an isothermal method only varying modulation period and amplitude and a non-isothermal method including an underlying linear heating ramp. Three different test compounds were investigated including a blank of NaCl, a small pharmaceutically active molecule (Valsartan) and a polymer (PVP-VA 64). Obtained optimum values were found to be identical for each compound tested and shown to be statistically robust for repeated daily experimentation. Optimized signals showed lower glass transition values T(g) paired with higher changes in isobaric heat capacity Δc(p). Measured glass transition signals exhibited minimal variation during repeat analysis, and showed significantly better signal-to-noise ratios in comparison to literature data.     

Biological evaluation of Fe₃O₄-poly(L-lactide)-poly(ethylene glycol)-poly(L-lactide) magnetic microspheres prepared in supercritical CO₂

Traditional gold mining, using metallic mercury (Hg(0)) to form gold amalgam, followed by burning to remove the Hg(0), is widely used in South America, Africa and Asia. The gold is sold to merchants who burn it again to eliminate remaining Hg(0). In Ecuador, 200 gold miners, 37 gold merchants and 72 referents were studied. The median Hg concentrations in urine (U-Hg) were 3.3 (range 0.23-170), 37 (3.2-420), and 1.6 (0.2-13)μg/g creatinine, respectively, and in whole blood (B-Hg) were 5.2, 30, and 5.0 μg/L, respectively. Biomarker concentrations among merchants were statistically significantly higher than among miners and referents; also the miners differed from the referents. Burning of gold amalgam among miners was intermittent; U-Hg decreased in the burning-free period. In computerized neuromotor examinations, B-Hg and U-Hg concentrations were associated with increases in the centre frequency of the tremor, as well as in reaction time and postural stability.Retention of Hg (B-Hg), and the elimination rate (U-Hg) appears to be modified by polymorphism in a gene of an enzyme in the glutathione synthesis (GCLM), but there were no significant genetic modifications for the associations between exposure and neurotoxicity.Thus, the gold merchants have a much higher exposure and risk than the miners, in whom the exposure varies over time. The metabolism of Hg is modified by genetic traits. The present exposure to Hg had limited neurotoxic effects.     

Characteristics of felodipine-located poly(ε-caprolactone) microspheres

Felodipine-loaded poly (ε-caprolactone) (PCL) microspheres were prepared by two methods, the conventional emulsion solvent evapouration method and the quenching method. The aim of this work was to investigate the effects of process parameters such as emulsion type, drug loading, molecular-weight of the polymer, types of emulsion stabilizer and dispersed phase solvents, as well as preparation methods. The results show that, when conventional emulsion solvent evapouration method was used, the o/w-method produced smaller mean size and higher encapsulation efficiency compared with the o/o-method. The encapsulation efficiencies increased with an increase in the molecular weight and a decrease in crystallinity of PCL. The size of microspheres varied with the type of emulsion stabilizer used, smaller microspheres with PVA and narrow size distribution with Pol 237. The water solubility of the dispersed phase solvent was one of the critical factors in controlling the encapsulation efficiency and microsphere mean size. When water-soluble solvents such as acetonitrile and ethyl formate were used, the encapsulation efficiencies decreased due to higher evapouration rate. When quenching methods were used, in contrast to the conventional emulsion solvent evapouration method, very narrowly size-distributed but bigger microspheres were obtained.     

Hydrocortisone-loaded poly(ε-caprolactone) nanoparticles for atopic dermatitis treatment

Atopic dermatitis (AD) is a chronic inflammatory skin condition that affects mostly young infants. The purpose of this research was to achieve a prolonged drug release and the reduction of side effects with hydrocortisone-loaded nanoparticles (NPs), for AD treatment. Poly(ε-caprolactone) (PCL) NPs were prepared by modified solvent displacement method and were characterized in terms of size, potential zeta, morphology, entrapment efficiency (EE), Fourier transform infrared (FT-IR) spectrometry and in vitro permeation studies using Franz cells. Toxicology of this nanosystem was also assessed. The obtained NPs EE showed an increased size and a more homogenous size distribution after loading and were negatively charged. EF was around 62%. In vitro release studies demonstrated a controlled release of drug from the NPs over time. FT-IR analysis showed the system stability for one week. Permeation studies revealed significant differences in the permeation of encapsulated and free hydrocortisone. In vitro toxicity studies showed no effect of drug toxicity after encapsulation. The study seems to indicate that encapsulation of hydrocortisone in PCL NPs could enable a faster control of the disease and a decrease in the side effects associated to the long-term application of corticosteroids.     

Accelerated Degradation of Poly(ε-caprolactone) by Organic Amines

The solid-state degradation of poly(-caprolactone) catalyzed by primary, secondary and tertiary alkylamines was investigated. The degradation process was monitored by weight loss and molecular weight change measured by gel permeation chromatography. Degradation studies were conducted at 37°C in methanol solutions of the alkylamines. Primary alkylamines caused rapid weight loss (i.e., ~90% weight loss in 30 days) that depended on alkylamine concentration, molar ratio of alkylamine to poly(-caprolactone) monomer and alkyl chain length. The secondary alkylamines caused less rapid polymer weight loss (i.e., ~90%) weight loss within 80 days). One tertiary alkylamine (N,N-diisopropylethylamine) showed little catalytic effect while a bicyclic tertiary alkylamine (quinuclidine) was about as catalytic as the primary alkylamines. The degradation products isolated when primary alkylamines were used include both esters and amides indicating that nucleophilic attack by the alkylamines competed with the amine-catalyzed methanolysis reaction. Only ester moieties could be identified in the products from reactions containing secondary and tertiary alkylamines, which indicated that they acted as nucleophilic catalysts. All of the primary alkylamines reduced poly(-caprolactone) molecular weight from about 25,000 to 10,000 within 10 days after which the molecular weight of the remaining solid leveled off even though weight loss continued.     

Surfactant-free microspheres of Poly(ε-caprolactone)/poly (ethylene glyco I )/poly(ε-caprolactone) triblock copolymers as a protein carrier

The aim of this study is to prepare biodegradable microspheres without the use of surfactants or emulsifiers for a novel sustained delivery carriers of protein drugs. A poly(epsilon-caprolactoney poly(ethylene glycol)/poly(epsilon-caprolactone) (CEC) triblock copolymer was synthesized by the ring-opening of epsilon-caprolactone with dihydroxy poly (ethylene glycol) to prepare surfactant-free microspheres. When dichloromethane (DCM) or ethyl formate (EF) was used as a solvent, the formation of microspheres did not occur. Although the microspheres could be formed prior to lyophilization under certain conditions, the morphology of microspheres was not maintained during the filtration and lyophilization process. Surfactant-free microspheres were only formed when ethyl acetate (EA) was used as the organic solvent and showed good spherical microspheres although the surfaces appeared irregular. The content of the protein in the microsphere was lower than expected, probably because of the presence of water channels and pores. The protein release kinetics showed a burst release until 2 days and after that sustained release pattern was showed. Therefore, these observations indicated that the formation of microsphere without the use of surfactant is feasible, and, this the improved process, the protein is readily incorporated in the microsphere.     

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Abstract

Context: Methotrexate (MTX) is used in the treatment of malignancies; however, its clinical application is limited by its toxic dose-related side effects. An alternative to overcome the toxicity of the MTX in healthy tissues is the design of an implantable device capable of controlling the delivery of this drug for an extended period within the tumor site.

Objective: To develop methotrexate-loaded poly(ε-caprolactone) implants (MTX PCL implants) and to demonstrate their efficacy as local drug delivery systems capable of inhibiting Ehrlich solid tumor bearing mice.

Materials and methods: MTX PCL implants were produced by the melt-molding technique and were characterized by FTIR, WAXS, DSC and SEM. The in vitro and in vivo release of MTX from the PCL implants was also evaluated. The efficacy of implants in inhibiting tumor cells in culture and the solid tumor in a murine model was revealed.

Results and discussion: The chemical and morphological integrity of the drug was preserved into the polymeric matrix. The in vitro and in vivo release processes of the MTX from the PCL implants were modulated by diffusion. MTX diffused from the implants revealed an antiproliferative effect on tumor cells. Finally, MTX controlled and sustained released from the polymeric implants efficiently reduced 42.7% of the solid tumor in mice paw.

Conclusion: These implantable devices represented a contribution to improve the efficacy and safety of chemotherapy treatments, promoting long-term local drug accumulation in the targeted site.     

Functionalized three-arm poly(ε-caprolactone) maleic acid microspheres for controlled protein release

Introduction

The objective of this work was to fabricate a novel class of protein carriers from double-bond-functionalized multiarm poly(ε-caprolactone) maleic acid (PGCLM) microspheres and to examine protein sustained-release profiles in vitro over a period of a few months.

Methods

The double-emulsion technique was used to formulate terminal functionalized three-arm PGCLM microspheres having three different types of functional groups (-OH, -COOH, and -C = C-), and one of the functional groups (>C = C< bonds) was used to formulate surface-crosslinked microspheres (NPGCLM). Ovalbumin (OVA) was used as a model protein for examining its release profiles from PGCLM and NPGCLM microspheres in 0.1M phosphate-buffered saline (PBS) at 37°C. These microspheres were also characterized in terms of their morphology, size distribution, and stability.

Results

The mean size of fabricated microspheres ranged from 21.9µm to 51.1µm. An OVA protein was successfully encapsulated into these biodegradable PGCLM microspheres with loading efficiency ranging from 34.2% to 46% (w/w), depending on the ratio of PGCLM to polyvinyl alcohol (PVA) stabilizer. Depending on the polymer to PVA stabilizer ratio, the cumulative OVA release % (w/w) in 0.1M PBS at 37°C ranged from 30% to 40% within 50 days. We further demonstrated the availability of the functional >C = C< bonds on the surface of PGCLM microspheres, which we expect could be used for either covalent binding of bioactive agents or imparting different chemical characteristics onto the surface of the microspheres for broadening of their applications.

Discussion/Conclusion

A method for the preparation of biodegradable microspheres from water/oil emulsion of multiarm and functionalized poly(ε-caprolactone) [PGCL, PGCLM, and NPGCLM] was reported as a potential means of developing injectable therapeutic formulations for drugs. The most unique aspect of these biodegradable microspheres is the availability of two functional groups (>C = C< bonds and -COOH pendant group) on the microsphere surface for potential additional chemical or/and biochemical modifications, such as the formation of crosslinked network surface structure. The incorporation of terminal hydrophilic functional maleic acid into hydrophobic three-arm PGCL chains significantly improved the loading efficiency of OVA and its release profiles. These functionalized biodegradable microspheres may provide a good alternative to linear aliphatic polyester-based drug delivery systems and resulted in development of a long-acting, injectable drug carrier for sustained drug release over a period of few months.     

Silk coating on poly(ε-caprolactone) microspheres for the delayed release of vancomycin

The treatment of osteomyelitis remains a challenge for orthopaedic surgeons. Controlled release of vancomycin from biodegradable microspheres is a promising method for eliminating infection. However, the large initial burst release may make it difficult to maintain the local vancomycin concentration superior to minimum inhibitory concentration for several weeks. The aims of this study were to explore applications of the silk fibroin (SF) as an aqueous coating material for vancomycin-loaded poly(ε-caprolactone) (PCL) microspheres, and investigate the effects of silk coating on in vitro drug release. Examinations of particle size analyses, vancomycin content, Fourier transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy and in vitro drug release were performed. The results showed that silk coating could reduce the large initial burst release and retard the vancomycin release. Therefore, we suggest that the SF could be used as an aqueous coating material for vancomycin-loaded PCL microspheres and prolonged the drug release. SF coating on vancomycin-loaded PCL microspheres may be considered as an effective approach to prolong the drug release and improve the anti-infection effects.     

Silk coating on poly(ε-caprolactone) microspheres for the delayed release of vancomycin

The treatment of osteomyelitis remains a challenge for orthopaedic surgeons. Controlled release of vancomycin from biodegradable microspheres is a promising method for eliminating infection. However, the large initial burst release may make it difficult to maintain the local vancomycin concentration superior to minimum inhibitory concentration for several weeks. The aims of this study were to explore applications of the silk fibroin (SF) as an aqueous coating material for vancomycin-loaded poly(ε-caprolactone) (PCL) microspheres, and investigate the effects of silk coating on in vitro drug release. Examinations of particle size analyses, vancomycin content, Fourier transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy and in vitro drug release were performed. The results showed that silk coating could reduce the large initial burst release and retard the vancomycin release. Therefore, we suggest that the SF could be used as an aqueous coating material for vancomycin-loaded PCL microspheres and prolonged the drug release. SF coating on vancomycin-loaded PCL microspheres may be considered as an effective approach to prolong the drug release and improve the anti-infection effects.